Applications of Targeted Protein Degradation in Drug Discovery
Applications of Targeted Protein Degradation in Drug Discovery
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发表时间：
2021
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通讯作者：
Xue;J. Jin
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作者：
Xue;J. Jin
蛋白质平衡是一个控制活细胞中蛋白质丰度的过程，以便在细胞和器官水平上维持健康的蛋白质组。在真核生物中，泛素-蛋白酶体途径和溶酶体网络是实现这一目的的两个主要系统。自从2001年首次尝试利用蛋白质降解原理设计药物以来，在过去的20年里取得了快速的进展。在这篇综述文章中，我们将总结几种蛋白质降解药物的设计方法，包括PROTAC、HOMO-PROTAC、OPTO-PROTAC、PHOTAC、CLIPTAC、ATTEC、AUTAC以及LYTAC，并简要讨论它们的最新进展。
Proteostasis is a process that controls protein abundance in living cells in order to maintain healthy proteome at both cell and organ levels. In eukaryotes, the ubiquitin-proteasome pathway and the lysosomal network are two main systems for this purpose. Since the first attempt was tried to design drugs using protein degradation principles in 2001, rapid progress has been made over the past 20 years. In this review article, we will summary a few approaches to design protein degradation drugs, including PROTACs, Homo-PROTACs, Opto-PROTACs, PHOTACs, CLIPTACs, ATTEC, AUTACs, as well as LYTACs, and briefly discuss their current progression.